APD668
- Product Name
- APD668
- CAS No.
- 832714-46-2
- Chemical Name
- APD668
- Synonyms
- APD668;CS-1179;APD 668, >=98%;APD 668; APD-668;APD668, 10 mM in DMSO;isopropyl 4-(1-(2-fluorine-4-(carbosulfonyl)phenyl)-1H-pyrazolo[3,4-D]pyrimidine-4-oxy)piperidine-1-carboxylate;4-[[1-(2-Fluoro-4-methylsulfonylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester;1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester;Inhibitor,CYPs,APD668,diabetes,Cytochrome P450,APD-668,GPR119,Potassium Channel,coupled,G-protein,steatohepatitis,CYP2C9,G Protein-Coupled Receptor 119,inhibit,KcsA;isopropyl 4-((1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)piperidine-1-carboxylate APD668
- CBNumber
- CB62667083
- Molecular Formula
- C21H24FN5O5S
- Formula Weight
- 477.51
- MOL File
- 832714-46-2.mol
APD668 Property
- Boiling point:
- 611.6±55.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥17.4 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic
- form
- solid
- pka
- 2.13±0.30(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 17642
- Product name
- APD668
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 17642
- Product name
- APD668
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $202
- Updated
- 2024/03/01
- Product number
- 17642
- Product name
- APD668
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $363
- Updated
- 2024/03/01
- Product number
- A726235
- Product name
- APD668
- Packaging
- 10mg
- Price
- $265
- Updated
- 2021/12/16
- Product number
- A726235
- Product name
- APD668
- Packaging
- 25mg
- Price
- $530
- Updated
- 2021/12/16
APD668 Chemical Properties,Usage,Production
Uses
APD 668 is a potent agonist of GPR119, a glucose-dependant insulinotropic receptor expressed in pancreatic β-cells and intestinal L-cells.
in vivo
APD668 (10-30 mg/kg; p.o. once daily for 8 weeks) significantly reduces blood glucose and glycated hemoglobin (HbA1c) levels, with no desensitization of the acute drug response[1].
APD668 (1-10 mg/kg; a single p.o.) markedly reduces blood glucose levels during oral glucose tolerance test in a dose-dependent manner in mice[1].
APD668 (0.08 mg/kg/min; i.v.) shows no effect during euglycemic condition, but significantly stimulates insulin release when blood glucose levels are raised to approximately 300 mg/dl in a hyperglycemic clamp model in the Sprague-Dawley rat[1].
APD668 (p.o.) exhibits rapid to moderate absorption (tmax≤2 h) in mice, rats, and monkeys, but slower in dogs (tmax=6 h), and moderate to good absolute oral bioavailability (44-79%) in mice, rats, and monkeys, but lower in dogs (22%)[1].
| Animal Model: | Male Zucker Diabetic Fatty (ZDF) rats (6 weeks old, 200-250 g)[1] |
| Dosage: | 10, 30 mg/kg |
| Administration: | P.o. once daily for 8 weeks |
| Result: | Decreased the blood glucose and HbA1c levels at 30 mg/kg/day. Did not develop diabetes, whereas the vehicle treated rats did. |
IC 50
hGPR119: 2.7 nM (IC50); rGPR119: 33 nM (IC50); CYP2C9: 0.1 μM (Ki); hERG channel: 3 μM (IC50)
References
[1]. semple g, ren a, fioravanti b, et al. discovery of fused bicyclic agonists of the orphan g-protein coupled receptor gpr119 with in vivo activity in rodent models of glucose control. bioorg med chem lett, 2011, 21(10):3134-41.
[2]. soga t, ohishi t, matsui t, et al. lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan g-protein-coupled receptor. biochem biophys res commun, 2005, 326(4):744-51.
[3]. overton ha, babbs aj, doel sm, et al. deorphanization of a g protein coupled receptor for oleoylethanolamide and its use in the discovery of small molecule hypophagic agents. cell metab, 2006, 3(3):167-75.
APD668 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from APD668 manufacturers
- Product
- ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE 832714-46-2
- Price
- US $1.00/ASSAYS
- Min. Order
- 1ASSAYS
- Purity
- 98%
- Supply Ability
- 10kg
- Release date
- 2019-09-04